Faculty of Chemistry, Razi University, Kermanshah, Iran.
Faculty of Chemistry, Razi University, Kermanshah, Iran.
Int J Biol Macromol. 2024 Jan;254(Pt 1):127728. doi: 10.1016/j.ijbiomac.2023.127728. Epub 2023 Oct 28.
Nowadays, one of the most important reasons of death in the world is cancer. With the development of nanotechnology, advanced methods for treatment of cancer have introduced. In this work, the fluorescent carbon dots (CDs) were prepared from chitosan as the second abundant polysaccharide present in the nature. The surface of CDs was modified with chitosan (CDs/CS) and then the amino groups of chitosan were conjugated with activated folic acid (CDs/CS-FA) for controlled delivery of doxorubicin (DOX) as anticancer drug against HeLa cancer cells. The DOX loading efficiency of fluorescent CDs/CS-FA was high and nearly 60 %. Due to pH sensitive swelling/deswelling of CS, the percentage of cumulative DOX release could reach 90 % at cancer tissue (pH of 5.0) and 52 % at normal tissue (pH of 7.4) within 30 h. The cytotoxicity study revealed that the synthesized CDs were highly compatible on HeLa cells with cell viability 97-88 %. Cellular imaging shows that the entry of CDs/CS-FA to HeLa cells causes a green fluorescence, while the CDs/CS without FA have a negligible fluorescence. These results are due to the important role of FA in cell internalization. Thus, the CDs/CS-FA nanocarrier is suitable candidate for controlled pH sensitive drug delivery and cellular imaging.
如今,世界上最重要的死亡原因之一是癌症。随着纳米技术的发展,已经引入了治疗癌症的先进方法。在这项工作中,从壳聚糖中制备了荧光碳点 (CDs),壳聚糖是自然界中第二丰富的多糖。CDs 的表面用壳聚糖进行了修饰 (CDs/CS),然后壳聚糖的氨基与活性叶酸 (CDs/CS-FA) 缀合,以作为抗癌药物阿霉素 (DOX) 进行控释,用于治疗 HeLa 癌细胞。荧光 CDs/CS-FA 的 DOX 负载效率很高,接近 60%。由于 CS 的 pH 敏感溶胀/收缩,在 30 小时内,在癌症组织(pH 值为 5.0)时,累积 DOX 释放的百分比可达 90%,在正常组织(pH 值为 7.4)时,累积 DOX 释放的百分比可达 52%。细胞毒性研究表明,合成的 CDs 对 HeLa 细胞具有高度相容性,细胞活力为 97-88%。细胞成像显示,CDs/CS-FA 进入 HeLa 细胞会导致绿色荧光,而没有 FA 的 CDs/CS 则几乎没有荧光。这些结果归因于 FA 在细胞内化中的重要作用。因此,CDs/CS-FA 纳米载体是适合用于 pH 敏感药物控释和细胞成像的候选物。